Bicycle Radionuclide Conjugates (BRCs) as agents for tumour targeting

Figure 9:Whole-body maximum intensity projections of 150 pmol 68 Ga-labeled BRC1 (A) and optimized BRC4 (B) in HT1080 tumor-bearing BALB/c nu/nu mice (right flank) 60 min p.i. obtained from small animal PET/MR imaging. HIGH TUMOUR UPTAKE, LOW HEALTHY TISSUE UPTAKE Bicycle molecules are suitable vectors for delivering radionuclides to tumours due to their favourable pharmacokinetic properties (specific tumour uptake, rapid penetration and rapid renal clearance). Due to their rapid clearance from blood circulation and minimal non-specific uptake into healthy tissue (apart from kidneys), they can be used effectively as diagnostic PET agents. The biodistribution profile of the Bicycle RadionuclideConjugates (BRCs) can be optimised to maintain high tumour uptake whilst significantly reducing kidney levels. BRCs emerge as promising agents for a theranostic approach.